2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid Receptor

Cannabinoid Receptor

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Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol.

Cannabinoid Receptor Isoform Specific Products:

Cannabinoid Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-119744
    BAY 38-7271
    		Agonist
    BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
    BAY 38-7271
  • HY-100328
    CB2R-IN-1
    		Inhibitor
    CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM.
    CB2R-IN-1
  • HY-150056
    CB1R Allosteric modulator 3
    		Modulator 98.05%
    CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively.
    CB1R Allosteric modulator 3
  • HY-118245
    APP-FUBINACA
    		Agonist
    APP-FUBINACA is a cannabinoid receptor agonist and a derivative of phenylalaninamide-based indazole-3-carboxamide. APP-FUBINACA exhibits neurostimulatory effects.
    APP-FUBINACA
  • HY-149644
    CB2R agonist 3
    		Agonist
    CB2R agonist 3 is an agonist of cannabinoid receptor 2 (CB2R), with EC50 of 0.37μM that plays an important role in immune system.
    CB2R agonist 3
  • HY-W751734
    HU 433
    		Agonist
    HU 433 is a synthetic cannabinoid CB2 receptor agonist and is the enantiomer of HU 308 (HY-161510). HU 433 exerts its anti-inflammatory and neuroprotective effects by binding to CB2 receptors. HU 433 can be used in the study of neuroinflammation and retinal diseases.
    HU 433
  • HY-122281
    JTE 7-31
    		Agonist
    JTE 7-31 selectively acts on peripheral cannabinoid receptors, minimizing central nervous system side effects. They exhibit potent immunomodulatory, anti-inflammatory and anti-allergic properties, as well as inhibitory effects on nephritis.
    JTE 7-31
  • HY-W705168
    Yangonin-d3
    Yangonin-d3 is the deuterium labeled Yangonin (HY-N0919). Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
    Yangonin-d<sub>3</sub>
  • HY-178448
    EGFR-IN-178
    		Activator
    EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC).
    EGFR-IN-178
  • HY-116380
    CB2 receptor antagonist 5
    CB2 receptor antagonist 5 (compound 4A) is a ligand of CB2 receptor with antagonist effect.
    CB2 receptor antagonist 5
  • HY-14160
    CB2 receptor agonist 7
    		Agonist
    CB2 receptor agonist 7 (Compound 5B) is a cannabinoid 2 (CB2) receptor agonist with blood-brain barrier permeability.
    CB2 receptor agonist 7
  • HY-W777527
    AM404-d4
    AM404-d4 is the deuterium labeled AM404 (HY-101388). AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC50 values in the low micromolar range. AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 μM). Neuroprotective Effect.
    AM404-d<sub>4</sub>
  • HY-14136S
    Rimonabant-d10
    		Antagonist
    Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
    Rimonabant-d<sub>10</sub>
  • HY-164913
    PSB-SB-1203
    		Modulator
    PSB-SB-1203 (Compound 25b) is a dual CB1/CB2 ligand that blocks CB1 but activates CB2 receptors (CB1 Ki 0.244 μM; CB2 Ki 0.210 μM, EC50 0.054 μM). PSB-SB-1203 is promising for research of obesity and cancers.
    PSB-SB-1203
  • HY-100778
    SMM-189
    		Agonist
    SMM-189 is  a potent and selective cannabinoid receptor 2 (CB2) inverse agonist. SMM-189 plays an important role in neurodegenerative disorders and traumatic brain injury research.
    SMM-189
  • HY-175666
    ISAM-CG557
    		Agonist
    ISAM-CG557 is a selective CB2R agonist, with a Ki of 54.6 nM. ISAM-CG557 reduces intracellular ROS levels and caspase activity. ISAM-CG557 exhibits significant MAPK bias and moderate G-protein bias, with CB2R EC50s of 0.60 nM (cAMP), 60.9 nM (β-arrestin) and 0.03 nM (MAPK). ISAM-CG557 exerts potent anti-inflammatory effects by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. ISAM-CG557 can be used for the study of neuroinflammatory and neurodegenerative disorders.
    ISAM-CG557
  • HY-155967
    CB1R/AMPK modulator 1
    		Antagonist
    CB1R/AMPK modulator 1 (Compound 38-S) is an orally active CB1R/AMPK modulator, with an Ki of 0.81 nM and an IC50 of 3.9 nM for CB1R. CB1R/AMPK modulator 1 activates AMPK. CB1R/AMPK modulator 1 reduces food intake and body weight, and improves glucose tolerance and insulin sensitivity.
    CB1R/AMPK modulator 1
  • HY-173083
    MDA7
    		Agonist
    MDA7 is the selective agonist for cannabinoid receptor 2 with EC50 of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models.
    MDA7
  • HY-118656
    Cannabicitran
    		Ligand
    Cannabicitran is a cannabinoid. Cannabicitran can decrease intraocular pressure in rabbits.
    Cannabicitran
  • HY-169820
    CE-178253 benzenesulfonate
    		Antagonist
    CE-178253 benzenesulfonate is a CB1 antagonist with central nervous system activity.
    CE-178253 benzenesulfonate
Cat. No. Product Name / Synonyms Application Reactivity
Cannabinoid Receptor Isoform Comparison

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